2135765-21-6

Name	Benz[a]indolo[2,3-g]quinolizine-9(6H)-methanol, 5,8,14,14a-tetrahydro-2,12-dimethoxy-3-(phenylmethoxy)-
CAS	2135765-21-6
Molecular Formula	C29H30N2O4
Molecular Weight	470.56
MOL File	2135765-21-6.mol

Synonyms

DC371739 Benz[a]indolo[2,3-g]quinolizine-9(6H)-methanol, 5,8,14,14a-tetrahydro-2,12-dimethoxy-3-(phenylmethoxy)-

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Chemical Properties

Boiling point	654.2±55.0 °C(Predicted)
density	1.29±0.1 g/cm3(Predicted)
form	Solid
pka	14.30±0.10(Predicted)
color	Light yellow to light brown

Hazard Information

Uses

DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. DC371739 decreases the protein expression of PCSK9 and increases the protein expression of LDLR. DC371739 has the potential for the research of hyperlipidemia[1][2].

in vivo

DC371739 (10, 30, 100 mg/kg; p.o.; daily for 21 days) decreases the plasma levels of total cholesterol (TC), LDL-cholesterol (LDL-C) and triglyceride in hamsters^[2].

Animal Model:	Six-week-old healthy male Syrian golden hamsters (HFD-fed) ^[2]
Dosage:	10, 30, 100 mg/kg
Administration:	P.o.; daily for 21 days
Result:	Decreased the serum TC levels of the hamsters treated with 10, 30, or 100 mg/kg by 29.46%, 35.65%, and 38.69%, the serum LDL-C levels were significantly lower by 23.25%, 31.04%, and 35.03%, respectively, led to significantly lower serum TG levels by 49.57%, 57.52%, and 78.16%.

References

[1] Bao X, et al. Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside. Signal Transduct Target Ther. 2024 Jan 8;9(1):13. DOI:10.1038/s41392-023-01690-3
[2] Wang J, et al. Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial. Cell Metab. 2022 May 3;34(5):667-680.e6. DOI:10.1016/j.cmet.2022.03.006

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